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- W2888777717 abstract "Chagas disease and Human African trypanosomiasis (HAT) are important public health issues in Latin American and sub-Saharan African countries, respectively, and are responsible for a significant number of deaths. The drugs currently used to treat Chagas disease and HAT present efficacy, toxicity, and/or resistance issues; thus, there is a clear need for the discovery of novel targets and drug candidates to combat these diseases. In recent years, much effort has been made to find inhibitors of cruzain and rhodesain, which are promising targets for the design of novel trypanocidal compounds, since they are essential for parasite survival. Many reviews covering the design of novel cruzain and rhodesain inhibitors have been published; however, none have focused on the chemistry of the inhibitors. Thus, in the present work we reviewed the synthetic strategies and routes for the preparation of relevant classes of cruzain and rhodesain inhibitors. Perhaps the most important are the vinyl sulfone derivatives, and a very efficient synthetic strategy based on the Horner–Wadsworth–Emmons reaction was developed to yield these compounds. Modern approaches such as the asymmetric addition of substituted ethynyllithium to N-sulfinyl ketimines were used to produce the chiral alkynes that were employed in the preparation of important chiral triazole derivatives (potent cruzain inhibitors) and chiral HPLC resolution was used for the preparation of enantiopure 3-bromoisoxazoline derivatives (rhodesain inhibitors). Moreover, we also highlight the most important activity results and updated SAR results." @default.
- W2888777717 created "2018-09-07" @default.
- W2888777717 creator A5000748300 @default.
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- W2888777717 creator A5057144159 @default.
- W2888777717 creator A5069635863 @default.
- W2888777717 creator A5077265764 @default.
- W2888777717 date "2018-09-01" @default.
- W2888777717 modified "2023-10-15" @default.
- W2888777717 title "Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors" @default.
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- W2888777717 doi "https://doi.org/10.1016/j.ejmech.2018.08.079" @default.
- W2888777717 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30282318" @default.
- W2888777717 hasPublicationYear "2018" @default.
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